2805-53-0Relevant academic research and scientific papers
Rapid abnormal [3+2]-cycloaddition of isatinN,N′-cyclic azomethine imine 1,3-dipoles with chalcones
Yue, Guizhou,Dou, Zhengjie,Zhou, Zexi,Zhang, Li,Feng, Juhua,Chen, Huabao,Yin, Zhongqiong,Song, Xu,Liang, Xiaoxia,Wang, Xianxiang,Rao, Hanbing,Lu, Cuifen
supporting information, p. 8813 - 8817 (2020/06/08)
The rapid synthesis of novel dicyclic spiropyrrolidine was reported, using [3+2]-cycloaddition of isatinN,N′-cyclic azomethine imine 1,3-dipoles, generated from the condensation of substituted isatins and pyrazolidones, with chalcones in 2-5 min. The dicy
Synthesis, cyclooxygenase inhibition and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing methanesulphonyl pharmacophore
Abdellatif, Khaled R. A.,Elsaady, Mohammed T.,Abdel-Aziz, Salah A.,Abusabaa, Ahmed H. A.
, p. 1545 - 1555 (2016/10/09)
A new series of 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives 13a–p were synthesized via aldol condensation of 3/4-nitroacetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-methanesulfonylphenylhydrazine hydrochloride. All the synthesized compounds were evaluated for their cyclooxygenase (COX) inhibition, anti-inflammatory activity and ulcerogenic liability. All compounds were more potent inhibitors for COX-2 than COX-1. While most compounds showed good anti-inflammatory activity, compounds 13d, 13f, 13k and 13o were the most potent derivatives (ED50 = 66.5, 73.4, 79.8 and 70.5 μmol/kg, respectively) in comparison with celecoxib (ED50 = 68.1 μmol/kg). Compounds 13d, 13f, 13k and 13o (ulcer index = 3.89, 4.86, 4.96 and 3.92, respectively) were 4–6 folds less ulcerogenic than aspirin (ulcer index = 22.75) and showed approximately ulceration effect similar to celecoxib (ulcer index = 3.35). In addition, molecular docking studies were performed for compounds 13d, 13f, 13k and 13o inside COX-2 active site which showed acceptable binding interactions (affinity in kcal/mol ?2.1774, ?6.9498) in comparison with celecoxib (affinity in kcal/mol ?6.5330).
Synthesis and anti-inflammatory evaluation of new 1,3,5-triaryl-4,5-dihydro-1H-pyrazole derivatives possessing an aminosulphonyl pharmacophore
Abdellatif, Khaled R. A.,Abdelgawad, Mohamed A.,Elshemy, Heba A. H.,Alsayed, Shahinda S. R.,Kamel, Gehan
, p. 1932 - 1942 (2015/11/24)
A novel series of 2-pyrazoline derivatives 13a-l was synthesized via aldol condensation of 4-substituted acetophenones with appropriately substituted aldehydes followed by cyclization of the formed chalcones with 4-hydrazinobenzenesulfonamide hydrochlorid
Synthesis, antitubercular activity, and QSAR analysis of substituted nitroaryl analogs: Chalcone, pyrazole, isoxazole, and pyrimidines
Gupta, Revathi A.,Kaskhedikar, Satish G.
, p. 3863 - 3880 (2013/07/26)
In the present investigation, 4-nitroacetophenone, on condensation with appropriate aldehydes in ethanolic sodium hydroxide solution, yielded the corresponding chalcones. These corresponding chalcones were reacted with hydrazine hydrate, urea, thiourea, a
